| Company Name: |
SPIRO PHARMA |
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eric_feng1954@126.com |
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| | CP-640186 (hydrochloride) Basic information |
| Product Name: | CP-640186 (hydrochloride) | | Synonyms: | CP-640186 (hydrochloride);CP640186 HCl;CP-640186 hydrochloride, >=98%;CS-1253;(3R)-1'-(anthracene-9-carbonyl)-3-(morpholine-4-c
arbonyl)-1,4'-bipiperidine hydrochloride;HepG2,muscle fatty acid oxidation,Inhibitor,CP 640186,CP640186,C2C12,CP-640186,human fibroblasts,H460,muscle strips,CP 640186 hydrochloride,inhibit,ACC, Acetyl Coenzyme A Carboxylase,Acetyl-CoA Carboxylase,CP640186 hydrochloride;(R)-Anthracen-9-yl(3-(morpholine-4-carbonyl)-[1,4'-bipiperidin]-1'-yl)methanone hydrochloride;CP-640186 hydrochloride, 10 mM in DMSO | | CAS: | 591778-70-0 | | MF: | C30H36ClN3O3 | | MW: | 522.09 | | EINECS: | | | Product Categories: | | | Mol File: | 591778-70-0.mol |  |
| | CP-640186 (hydrochloride) Chemical Properties |
| storage temp. | Store at -20°C | | solubility | DMSO:39.0(Max Conc. mg/mL);74.7(Max Conc. mM)
H2O:50.0(Max Conc. mg/mL);95.77(Max Conc. mM) | | form | Solid | | color | Light yellow to pink | | Water Solubility | H2O: 2mg/mL, clear (warmed) |
| | CP-640186 (hydrochloride) Usage And Synthesis |
| Uses | CP 640186 Hydrochloride can be used as acetyl CoA carboxylase inhibitors against metabolic syndrome and other disorders. | | Biological Activity | CP-640186 is a potent and orally active acetyl-CoA carboxylase 1/2 (ACC-alpha/beta, ACC1/2) inhibitor (IC50 ~50 nM) th at targets the carboxyltransferase (CT) domain at the ACC dimer interface (via tight interactions with the putative biotin-binding site) in a reversible manner, uncompetitive with respect to ATP, and non-competitive with respect to bicarbonate, acetyl-CoA, and citrate. CP-610431 inhibits fatty acid (FA) synthesis, triglyceride (TG) synthesis, TG and apoB secretion (IC50 = 1.6, 1.8, 3.0, and 5.7 μM, respectively), but not cholesterol synthesis or apoC3 secretion in HepG2 cells (ACC1), as well as stimulates FA oxidation in C2C12 cells (ACC2) and in r at epitrochlearis muscle strips (EC50 = 57 nM and 1.3 μM, respectively). Oral administration is shown to inhibit FA synthesis in rats, CD1 mice, and ob/ob mice (ED50 = 13, 11, and 4 mg/kg, respectively) and stimulate r at whole body FA oxidation (ED50 ∼30 mg/kg) in vivo. | | in vivo | CP-640186 (oral gavage; 4.6-21 mg/kg; once) demonstrates acute efficacy[1].
CP-640186 (intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once) shows lowe drug exposure in the rat than the ob/ob mouse at equal doses[1].
CP-640186 (oral gavage; 100 mg/kg; once) treatment shows a complete shift from carbohydrate utilization to fatty acid utilization as a source of energy at high exposure level[1]. | Animal Model: | Male ob/ob mice[1] | | Dosage: | 4.6-21 mg/kg | | Administration: | Oral gavage; 4.6-21 mg/kg; once | | Result: | Demonstrated acute efficacy for up to 8 h after oral administration, exhibiting ED50 values of 4.6, 9.7, and 21 mg/kg, at 1, 4, and 8 h, respectively, after treatment. |
| Animal Model: | Male Sprague-Dawley rats[1] | | Dosage: | Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg | | Administration: | Intravenous injection and oral gavage; intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once | | Result: | Showed a plasma half-life of 1.5 h, a bioavailability of 39%, a Clp of 65 ml/min/kg, a Vdss of 5 liters/kg, an oral Tmax of 1.0 h, an oral Cmax of 345 ng/mL, and an oral AUC0-∞ of 960 ngh/mL. |
| Animal Model: | Male ob/ob mice[1] | | Dosage: | Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg | | Administration: | Intravenous injection and oral gavage; Intravenous dose, 5 mg/kg; oral dose, 10 mg/kg; once | | Result: | Showed a plasma half-life of 1.1 h, a bioavailability of 50%, a Clp of 54 ml/min/kg, an oral Tmax of 0.25 h, an oral Cmax of 2177 ng/mL, and an oral AUC0-∞ of 3068 ngh/mL. |
| Animal Model: | Twenty male Sprague-Dawley rats (350-400 g) fasted and then refed a high sucrose diet for 2 days; additional eight rats fasted for 24 h[1] | | Dosage: | 100 mg/kg | | Administration: | Oral gavage; 100 mg/kg; once | | Result: | Resulted in time-dependent reductions in RQ (a ratio of CO2 production to O2 consumption) of up to 64%. |
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| | CP-640186 (hydrochloride) Preparation Products And Raw materials |
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